1. Technical Field
Aspects of this document relate generally to n-acetyl beta alanine and methods of use.
2. Background
β-Alanine (or beta-alanine) is a naturally occurring beta amino acid, which are amino acids in which the amino group is at the β-position from the carboxylate group. Its structure is as follows:

β-Alanine is not used in the biosynthesis of any major proteins or enzymes. It is formed in vivo by the degradation of dihydrouracil and carnosine. It is a component of the naturally occurring peptides carnosine and anserine and also of pantothenic acid (vitamin B5) which itself is a component of coenzyme A. Under normal conditions, β-alanine is metabolized into acetic acid.
β-Alanine is the rate-limiting precursor of carnosine, which is to say carnosine levels are limited by the amount of available β-Alanine. Carnosine removes excess acid from the muscle cell, thus reducing fatigue, etc. Therefore, the beneficial effects described for beta-alanine also apply to carnosine. Supplementation with β-alanine has been shown to increase the concentration of carnosine in muscles, decrease fatigue in athletes and increase total muscular work done.
See for example the following publications. In “Muscle carnosine metabolism and beta-alanine supplementation in relation to exercise and training”, Derave et al., Sports Med. 2010 Mar. 1; 40(3):247-63, the researchers have made an extensive review of beta-alanine's physiological role, it's effects and it's ability to enhance sports performance. In “The effects of 10 weeks of resistance training combined with beta-alanine supplementation on whole body strength, force production, muscular endurance and body composition”, Kendrick et al., Amino Acids. 2008 May; 34(4):547-54 it was exhibited that beta alanine supplementation can enhance muscle carnosine levels. In “Beta-alanine supplementation reduces acidosis but not oxygen uptake response during high-intensity cycling exercise”, Baquet et al., Eur J Appl Physiol. 2010 February; 108(3):495-503, it was described that beta alanine supplementation at 4.8 grams per day can attenuate acidosis due to exercise, resulting in increased performance in some models.
β-Alanine, therefore, finds great use in sports supplements to reduce muscle fatigue, muscle damage, promote endurance, promote recovery, increase strength and improve athletic performance and body composition. Apart from these uses beta-alanine may be used for the treatment of muscle wasting diseases, in anti-aging formulas, in overall health formulas and any other use where increased muscular performance is wanted. The effective doses used in studies range from 2.4 grams per day (see for example, “The effect of beta-alanine supplementation on neuromuscular fatigue in elderly (55-92 Years): a double-blind randomized study”, Stout et al., Journal of the International Society of Sports Nutrition 2008, 5:21, where supplementation of 800 mg×3 per day resulted in 28% increase in physical working capacity fatigue threshold) to as much as 6 grams per day, although it is not uncommon to see supplements with lower (as little as 500 mg) or larger doses.
Despite the foregoing, beta alanine's use still suffers from drawbacks. The biggest drawback of beta alanine use is paresthesia, a “tingling” sensation users experience that comes from reaction of beta alanine with nerves of the skin. Symptoms of paresthesia start at doses as low as 800 mg (see, for example, “Role of beta-alanine supplementation on muscle carnosine and exercise performance”, Artioli et al., Med Sci Sports Exerc. 2010 June; 42(6):1162-73, where it is mentioned that “Symptoms of paresthesia may be observed if a single dose higher than 800 mg is ingested”) and can worsen with higher doses. This is so uncomfortable to some users that they opt to use beta alanine in many small servings during the day or just not all.
Another drawback of beta alanine is that while it is water soluble, it is very poorly soluble in organic solvents. Beta alanine is described to have a water solubility of 55-89 grams/100 ml. This makes it extremely hydrophilic and lipophobic, which may hinder it's capacity to bypass certain cell membranes like the blood-brain barrier (see, for example, “Determination of lipophilicity and its use as a predictor of blood-brain barrier penetration of molecular imaging agents”, Waterhouse, Mol Imaging Biol. 2003 November-December; 5(6):376-89, where it is described how increasing lipophilicity increases blood-brain barrier permeation) or the muscle cell wall by passive diffusion. Although beta alanine is transported by an active transport system (see, for example, “Sodium and chloride ion-dependent transport of beta-alanine across the blood-brain barrier”, Komura et al., J. Neurochem. 1996 July; 67(1):330-5, where Komura et. al. describe how beta-alanine can be transported via the Blood Brain Barrier by a sodium/chloride dependent channel) it would be desirable to increase absorption rate by adding passive diffusion to the absorption mechanisms (increasing lipophilicity can increase permeation and absorption through biological membranes).